CA2703125C - Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer - Google Patents

Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer Download PDF

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Publication number
CA2703125C
CA2703125C CA2703125A CA2703125A CA2703125C CA 2703125 C CA2703125 C CA 2703125C CA 2703125 A CA2703125 A CA 2703125A CA 2703125 A CA2703125 A CA 2703125A CA 2703125 C CA2703125 C CA 2703125C
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Canada
Prior art keywords
pyrazol
pyrrolo
6alkyl
pyrazin
independently selected
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
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CA2703125A
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English (en)
French (fr)
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CA2703125A1 (en
Inventor
David J. Guerin
Joon Jung
Elizabeth Stanton
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Merck Sharp and Dohme LLC
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Publication of CA2703125A1 publication Critical patent/CA2703125A1/en
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Publication of CA2703125C publication Critical patent/CA2703125C/en
Expired - Fee Related legal-status Critical Current
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2703125A 2007-10-25 2008-10-21 Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer Expired - Fee Related CA2703125C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US34307P 2007-10-25 2007-10-25
US61/000,343 2007-10-25
PCT/US2008/011971 WO2009054941A1 (en) 2007-10-25 2008-10-21 Therapeutic compounds

Publications (2)

Publication Number Publication Date
CA2703125A1 CA2703125A1 (en) 2009-04-30
CA2703125C true CA2703125C (en) 2012-08-28

Family

ID=40579830

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2703125A Expired - Fee Related CA2703125C (en) 2007-10-25 2008-10-21 Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer

Country Status (6)

Country Link
US (1) US8183245B2 (hr)
EP (1) EP2211620B1 (hr)
JP (1) JP2011500806A (hr)
AU (1) AU2008317406B2 (hr)
CA (1) CA2703125C (hr)
WO (1) WO2009054941A1 (hr)

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ES2378513T3 (es) 2008-08-06 2012-04-13 Pfizer Inc. Compuestos 2-heterociclilamino piracinas sustituidas en posición 6 como inhibidores de CHK-1
US8877772B2 (en) 2008-11-25 2014-11-04 University Of Rochester Substituted pyrrolo[2,3-B]pyridines as MLK inhibitors
DE102009019962A1 (de) * 2009-05-05 2010-11-11 Merck Patent Gmbh 3-([1,2,3]Triazol-4-yl)-pyrrolo[2,3-b]pyridinderivate
SI2440558T1 (sl) * 2009-06-08 2015-10-30 Takeda Pharmaceutical Company Limited Spojine dihidropirolonaftiridinona kot inhibitorji JAK
EP2338888A1 (en) * 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
UY33213A (es) * 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
WO2011137022A1 (en) * 2010-04-27 2011-11-03 Merck Sharp & Dohme Corp. Azaindoles as janus kinase inhibitors
NZ603644A (en) 2010-05-24 2014-10-31 Univ Rochester Bicyclic heteroaryl kinase inhibitors and methods of use
WO2012054364A2 (en) * 2010-10-22 2012-04-26 Merck Sharp & Dohme Corp. Bicyclic diamines as janus kinase inhibitors
DE102010049877A1 (de) 2010-11-01 2012-05-03 Merck Patent Gmbh 7-((1,2,3)Triazol-4-yl)-pyrrolo(2,3) pyrazinderivate
EP2640699B1 (en) 2010-11-17 2015-10-07 Actelion Pharmaceuticals Ltd. Bridged spiro[2,4]heptane ester derivatives
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
DE102010053347A1 (de) * 2010-12-03 2012-06-06 Merck Patent Gmbh 3-Hetaryl-substituierte Pyrrolo[2,3-b] pyridin-derivative als PDK1-Inhibitoren
DE102011008352A1 (de) * 2011-01-12 2012-07-12 Merck Patent Gmbh 5-([1,2,3]Triazol-4-yl)-7H-pyrrolo-[2,3-d]pyrimidinderivate
DE102011009961A1 (de) 2011-02-01 2012-08-02 Merck Patent Gmbh 7-Azaindolderivate
AU2012232658B2 (en) 2011-03-22 2016-06-09 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
DE102011105469A1 (de) * 2011-06-24 2012-12-27 Merck Patent Gmbh 7-Azaindolderivate
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
DE102011119127A1 (de) 2011-11-22 2013-05-23 Merck Patent Gmbh 3-Cyanaryl-1H-pyrrolo[2.3-b]pyridin-Derivate
US9527851B2 (en) 2011-12-21 2016-12-27 Jiangsu Hengrui Medicine Co., Ltd. Pyrrole six-membered heteroaryl ring derivative, preparation method thereof, and medicinal uses thereof
CA2880896C (en) 2012-06-26 2021-11-16 Del Mar Pharmaceuticals Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof
WO2014013014A1 (en) 2012-07-18 2014-01-23 Fundació Privada Centre De Regulació Genòmica (Crg) Jak inhibitors for activation of epidermal stem cell populations
US9593115B2 (en) 2012-09-21 2017-03-14 Advinus Therapeutics Ltd. Substituted fused tricyclic compounds, compositions, and medicinal applications thereof
DE102012019369A1 (de) 2012-10-02 2014-04-03 Merck Patent Gmbh 7-Azaindolderivat
CN104884059B (zh) 2012-11-30 2018-08-10 罗切斯特大学 用于hiv/aids治疗的混合谱系激酶抑制剂
US11491154B2 (en) 2013-04-08 2022-11-08 Dennis M. Brown Therapeutic benefit of suboptimally administered chemical compounds
WO2015131080A1 (en) 2014-02-28 2015-09-03 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
TWI788655B (zh) 2015-02-27 2023-01-01 美商林伯士拉克許米公司 酪胺酸蛋白質激酶2(tyk2)抑制劑及其用途
JP6802263B2 (ja) * 2015-09-02 2020-12-16 ニンバス ラクシュミ， インコーポレイテッド Ｔｙｋ２阻害剤およびその使用
JP2019519579A (ja) 2016-06-30 2019-07-11 デウン ファーマシューティカル カンパニー リミテッド キナーゼ阻害剤としてのピラゾロピリミジン誘導体
WO2018041989A1 (en) 2016-09-02 2018-03-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for diagnosing and treating refractory celiac disease type 2
JP6937828B2 (ja) * 2016-11-23 2021-09-22 江蘇恒瑞医薬股▲ふん▼有限公司 ピロロ６員複素芳香環誘導体の製造方法、および中間体
EP3571198B1 (en) * 2017-01-20 2023-02-01 LEO Pharma A/S Bicyclic amines as jak kinase inhibitors
SI3762368T1 (sl) 2018-03-08 2022-06-30 Incyte Corporation Aminopirazin diolne spojine kot zaviralci PI3K-y
US10508113B2 (en) 2018-03-12 2019-12-17 Abbvie Inc. Inhibitors of tyrosine kinase 2 mediated signaling
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
JP2022527972A (ja) 2019-04-02 2022-06-07 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル 前悪性病変を有する患者において癌を予測及び予防する方法
CA3136224A1 (en) * 2019-04-09 2020-10-15 Plexxikon Inc. Condensed azines for ep300 or cbp modulation and indications therefor
US20220202820A1 (en) 2019-04-16 2022-06-30 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
WO2023222565A1 (en) 2022-05-16 2023-11-23 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stems cells induced by chronic inflammation

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EP1599475A2 (en) * 2003-03-06 2005-11-30 Eisai Co., Ltd. Jnk inhibitors
EP2332940B1 (en) 2004-03-30 2012-10-31 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of JAK and other protein kinases
US7361764B2 (en) * 2004-07-27 2008-04-22 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
CA2573362A1 (en) * 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
EP1828180A4 (en) 2004-12-08 2010-09-15 Glaxosmithkline Llc 1H-pyrrolo [2,3-BETA] PYRIDINE
US20060264442A1 (en) 2005-05-18 2006-11-23 Allergan, Inc. Methods for the treatment of ocular and neurodegenerative conditions in a mammal
NZ565255A (en) 2005-06-22 2010-04-30 Plexxikon Inc Pyrrolo[2,3-b] pyridine derivatives as protein kinase inhibitors
JP5071374B2 (ja) * 2005-07-14 2012-11-14 アステラス製薬株式会社 ヘテロ環ヤヌスキナーゼ３阻害剤
UA98449C2 (en) * 2005-12-13 2012-05-25 Инсайт Корпорейшин Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
CA2703125C (en) * 2007-10-25 2012-08-28 David J. Guerin Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer

Also Published As

Publication number Publication date
EP2211620A4 (en) 2012-06-06
US20100210623A1 (en) 2010-08-19
CA2703125A1 (en) 2009-04-30
EP2211620B1 (en) 2013-12-25
US8183245B2 (en) 2012-05-22
AU2008317406B2 (en) 2013-07-18
EP2211620A1 (en) 2010-08-04
JP2011500806A (ja) 2011-01-06
AU2008317406A1 (en) 2009-04-30
WO2009054941A1 (en) 2009-04-30

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